[11C]Yohimbine PET Study of alpha2-AR

NCT ID: NCT03520543

Last Updated: 2025-09-12

Basic Information

• Recruitment Status: COMPLETED
• Clinical Phase: PHASE1
• Total Enrollment: 16 participants
• Study Classification: INTERVENTIONAL
• Study Start Date: 2018-05-21
• Study Completion Date: 2019-01-21

Brief Summary

The main purpose of this study is to model tissue specific kinetics of [11C]Yohimbine in healthy male participants by positron emission tomography (PET) and the appropriate arterial input function (part A) ; to determine the reproducibility of measures (classical test-retest study, part B1) and to measure the blocking of [11C]Yohimbine uptake in the brain following single oral dose administration of clonidine (part B2).

Conditions

Healthy Controls

Study Design

• Allocation Method: RANDOMIZED
• Intervention Model: PARALLEL
• Primary Study Purpose: BASIC_SCIENCE
• Blinding Strategy: NONE

Study Groups

Part A : Imput function

Compartmental model of the volume of distribution of \[11C\]Yohimbine in Brain by PET

Group Type: EXPERIMENTAL

[11C]Yohimbine

Intervention Type: DRUG

Each subject will receive an intravenous (IV) bolus injection of \[11C\]Yohimbine at a dose of 370 MegaBecquerel (MBq) ± 10% with concomitant arterial blood sampling. The distribution of \[11C\]Yohimbine in brain will be measured by dynamic PET scans obtained from the time of injection for up to 90 minutes along with measurement of the tracer input function with arterial samples for intact tracer and metabolites to establish the total and regional compartmental kinetics of \[11C\]Yohimbine.

Part B : validity of the measure

Part B1 : Test Retest Variability in the distribution of \[11C\]Yohimbine Part B2 : Percentage of alpha2-adrenergic receptor occupancy

Group Type: EXPERIMENTAL

[11C]Yohimbine (Part B1) and [11C]Yohimbine + clonidine (Part B2)

Intervention Type: DRUG

Part B1 : Test Retest Variability will be assessed on percent difference in the binding potential following [11C]Yohimbine PET scan (IV bolus injection of [11C]Yohimbine at a dose of 370 MBq ± 10%) obtained at least 1 week after [11C]Yohimbine PET scan of part A.

Part B2 : Occupancy of alpha2-adrenergic receptors in brain by clonidine will be evaluated by comparing the binding potential of [11C]Yohimbine (IV bolus injection of [11C]Yohimbine at a dose of 370 MBq ± 10%) after single oral dose of clonidine (0,15mg) to the binding potential of [11C]Yohimbine obtained at baseline (part A).

Interventions

[11C]Yohimbine

Each subject will receive an intravenous (IV) bolus injection of \[11C\]Yohimbine at a dose of 370 MegaBecquerel (MBq) ± 10% with concomitant arterial blood sampling. The distribution of \[11C\]Yohimbine in brain will be measured by dynamic PET scans obtained from the time of injection for up to 90 minutes along with measurement of the tracer input function with arterial samples for intact tracer and metabolites to establish the total and regional compartmental kinetics of \[11C\]Yohimbine.

Intervention Type: DRUG

[11C]Yohimbine (Part B1) and [11C]Yohimbine + clonidine (Part B2)

Part B1 : Test Retest Variability will be assessed on percent difference in the binding potential following [11C]Yohimbine PET scan (IV bolus injection of [11C]Yohimbine at a dose of 370 MBq ± 10%) obtained at least 1 week after [11C]Yohimbine PET scan of part A.

Part B2 : Occupancy of alpha2-adrenergic receptors in brain by clonidine will be evaluated by comparing the binding potential of [11C]Yohimbine (IV bolus injection of [11C]Yohimbine at a dose of 370 MBq ± 10%) after single oral dose of clonidine (0,15mg) to the binding potential of [11C]Yohimbine obtained at baseline (part A).

Intervention Type: DRUG

Eligibility Criteria

Inclusion Criteria

• Healthy male volunteers
• Age between 20 years and 35 years
• Weight between 50kg and 90kg
• Without neurologic or psychiatric history
• Without head trauma history including loss of consciousness superior to 30 minutes.
• Affiliated to a social security or similar scheme
• Not subject to any legal protection measures
• Participant must have signed an informed consent document indicating that they understand the purpose of, and procedures required for, the study and are willing to participate in the study and comply with the study procedures and restrictions

Exclusion Criteria

• Allen test (assessing the arterial blood flow to the hand) indicating abnormal blood supply to the hand
• Subject with orthostatic hypotension
• Subject with alcohol or substance abuses history
• Subject with somatic drug therapies
• MRI contraindications (implanted or embedded metal objects in the head or body)
• PET contraindications
• Clonidine contraindications
• Exposed to 1 millisievert or more of ionizing radiation in the year before the start of this study
• Subject unable to sign written consent for participation in the study

• Minimum Eligible Age: 20 Years
• Maximum Eligible Age: 35 Years
• Eligible Sex: MALE
• Accepts Healthy Volunteers: Yes

Sponsors

Hospices Civils de Lyon

OTHER

Sponsor Role: lead

Responsible Party

Responsibility Role: SPONSOR

Principal Investigators

Chloe LAURENCIN, MD

Role: PRINCIPAL_INVESTIGATOR

Service de neurologie C

Locations

Service de Neurologie C - Hôpital Neurologique et Neurochirurgical Pierre Wertheimer, GHE

Bron, , France

Countries

France

References

Laurencin C, Lancelot S, Merida I, Costes N, Redoute J, Le Bars D, Boulinguez P, Ballanger B. Distribution of alpha2-Adrenergic Receptors in the Living Human Brain Using [11C]yohimbine PET. Biomolecules. 2023 May 15;13(5):843. doi: 10.3390/biom13050843.

Reference Type: RESULT

PMID: 37238713 (View on PubMed)

Other Identifiers

2018-000380-82

Identifier Type: EUDRACT_NUMBER

Identifier Source: secondary_id

69HCL17_0196

Identifier Type: -

Identifier Source: org_study_id